Flutamide

Androgen Receptor Antagonist

DB00499

Approved Indication

For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate

3 Targets

14 Resistance Mutations

21 References

3D Structure No structure available

No co-crystal structure available

Protein Targets

AR P10275 ✓ AHR P35869 NR1I2 O75469

Mechanism of Action

Flutamide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Flutamide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.

Resistance Mutations — 28 resistance samples observed in COSMIC

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p.H733Q p.H733R p.Q109* 1 p.Q451* p.Q641* 5 p.T346A p.T346S p.T695A p.T695S p.T878A 5 p.T878S 5 p.V184M p.V526M p.V716M 5

Resistance mutations sourced from COSMIC Drug Resistance database. Cyan = on-target · Amber = off-target · numbered badge = PubMed references for that mutation

Details

DrugBank ID DB00499 ↗

Approval Date 2001-09-18

Molecular Weight 276.2118 g/mol

Drug Class Androgen Receptor Antagonist

ATC Codes L02BB01

Synonyms Flutamid, Flutamida, Flutamide

PubChem CID: 3397 ↗

ChEMBL CHEMBL806 ↗

SMILES

CC(C)C(=O)NC1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F

ADMET Profile

Computing properties…